香豆素噻唑类化合物的合成及其抗菌活性研究

Synthesis and Antibacterial Activity of Coumarin Thiazole Derivatives

以水杨醛为原料,经5步反应合成了一系列新型香豆素噻唑类化合物,其结构经~1HNMR、^(13)CNMR和元素分析证实。体外考察了所得化合物对大肠杆菌、金黄色葡萄球菌和枯草芽孢杆菌的抑制活性。结果表明,大部分化合物都具有较强的抗菌活性。其中,化合物(E)-N'-(3-氟-4-羟基苯基亚甲基)-4-(2-氧代-2H-苯并吡喃-3-基)噻唑-2-酰肼活性最好,对大肠杆菌、金黄色葡萄球菌和枯草芽孢杆菌的最低抑制浓度分别为0.39、1.56和1.56μg/mL。

A series of novel coumarin thiazole derivatives were successfully synthesized via five steps,by using salicylaldehyde as raw material.The structures of the synthesized compounds were confirmed by ^1HNMR,^13CNMR and elemental analysis.The antibacterial activities against Escherichia coli,Staphylococcus aureus and Bacillus subtilis were tested.The majority of the screened compounds displayed potent antibacterial activity.Among them,（E）-N＇-（3-fluoro-4-hydroxybenzylidene）-4-（2-oxo-2H-chromen-3-yl） thiazole-2-carbohydrazide showed the most potent antibacterial activity against Escherichia coli,Staphylococcus aureus and Bacillus subtilis with minimum inhibitory concentration（MIC） of 0.39,1.56,1.56 μg/mL,respectively.